Evidence map›Paper›PMID 34528437›Full record

ArticleJournal of medicinal chemistry2021

Indole Chloropyridinyl Ester-Derived SARS-CoV-2 3CLpro Inhibitors: Enzyme Inhibition, Antiviral Efficacy, Structure-Activity Relationship, and X-ray Structural Studies.

Arun K Ghosh, Jakka Raghavaiah, Dana Shahabi, Monika Yadav, Brandon J Anson, Emma K Lendy, Shin-Ichiro Hattori, Nobuyo Higashi-Kuwata, Hiroaki Mitsuya, Andrew D Mesecar

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.

0numbers the graph read from it
0cells of the map it votes in
45citing papers in PubMed
5.0field-weighted citation impact, top 4% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

45 citing papers in PubMed, 89 citations in OpenAlex.

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  13. Advances in the Search for SARS-CoV-2 MPathogens (Basel, Switzerland) · 2024
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 2 institutions in 2 countries.

Arun K GhoshDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, Indiana 47907, United States.ORCID 0000-0003-2472-1841
Jakka RaghavaiahDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, Indiana 47907, United States.
Dana ShahabiDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, Indiana 47907, United States.
Monika YadavDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, Indiana 47907, United States.
Brandon J AnsonDepartment of Biological Sciences, Purdue University, West Lafayette, Indiana 47907, United States.
Emma K LendyDepartment of Biochemistry, Purdue University, West Lafayette, Indiana 47907, United States.
Shin-Ichiro HattoriDepartment of Refractory Viral Infections, National Center for Global Health and Medicine Research Institute, Shinjuku, Tokyo 162-8655, Japan.
Nobuyo Higashi-KuwataDepartment of Refractory Viral Infections, National Center for Global Health and Medicine Research Institute, Shinjuku, Tokyo 162-8655, Japan.
Hiroaki MitsuyaDepartment of Hematology and Infectious Diseases, Kumamoto University School of Medicine, Kumamoto 860-8556, Japan.
Andrew D MesecarDepartment of Biological Sciences, Purdue University, West Lafayette, Indiana 47907, United States.ORCID 0000-0002-1241-2577
Purdue University West Lafayette · USNational Center for Global Health and Medicine · JP

Funding

Transgenic Mouse Core Facility Shared Resource (TMCF-SR)P30CA023168 · NCI · PURDUE UNIVERSITY WEST LAFAYETTE · PI Andrea L Kasinski · 1985 to 2026
$43.4M
SARS-CoV-2 protease inhibitors for treating COVID-19R01AI158649 · NIAID · PURDUE UNIVERSITY · PI ARUN K GHOSH, ANDREW D MESECAR · 2021 to 2026
$3.8M
Design & Synthesis of Nonpeptide Protease InhibitorsR01AI150466 · NIAID · PURDUE UNIVERSITY · PI ARUN K GHOSH · 2023 to 2026
$2.4M
Design & Synthesis of Nonpeptide Protease InhibitorsR37AI150466 · NIAID · PURDUE UNIVERSITY · PI GHOSH, ARUN K · 2019 to 2020
$969k
NCI NIH HHS P30 CA023168NIAID NIH HHS HHSN272201700060CNIAID NIH HHS R01 AI150466NIAID NIH HHS R01 AI158649NIAID NIH HHS R37 AI150466
6 · The paper itself

Abstract

Here, we report the synthesis, structure-activity relationship studies, enzyme inhibition, antiviral activity, and X-ray crystallographic studies of 5-chloropyridinyl indole carboxylate derivatives as a potent class of SARS-CoV-2 chymotrypsin-like protease inhibitors. Compound

Indexed as

Adenosine MonophosphateAlanineAnimalsBinding SitesChlorocebus aethiopsCoronavirus 3C ProteasesCOVID-19Crystallography, X-RayHumansIndolesMolecular Dynamics SimulationProtease InhibitorsPyridinesSARS-CoV-2Structure-Activity RelationshipVero Cells3C-like proteinase, SARS-CoV-2Adenosine MonophosphateAlanineCoronavirus 3C ProteasesIndolesProtease InhibitorspyridinePyridinesremdesivir

Identifiers

PMID34528437
PMCPMC8457330
OpenAlexW3199998540

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.